Formulation and optimization of lipid- and Poloxamer-tagged niosomes for dermal delivery of terbinafine: preparation, evaluation, and in vitro antifungal activity.

ABSTRACT

Fungal skin diseases are recognized as a global burden disease that affect human quality adjusted life. Terbinafine belongs to allylamine and broad-spectrum antifungal drugs but considered practically insoluble. Different lipids/surfactant with two different molar ratios were investigated with Span 40-based niosomes; characterized for size, morphology, loading capacity (EE%), in vitro release, kinetics, and antifungal activities. Vesicle sizes (0.19-1.23 µm), EE% (25-99%), zeta potential (> -32 mV), and in vitro release rates were dependent on both lipid types and ratios. Higher ratios of Poloxamer 407 preferably formed mixed micelles rather than forming noisome bilayers. Both Compritol and Precirol were deemed to be potential alternatives to cholesterol as bilayer membrane stabilizers. Terbinafine-loaded Compritol and Precirol stabilized niosomes were successfully prepared and demonstrated superior antifungal activities in vitro (inhibition zones) using Candida albicans ATCC 60913.